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Merck - 5.08053.0001 - Mcl-1 Inhibitor II - Calbiochem

  • MFR SKU: 5.08053.0001
  • ITEM #: 17952435
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ITEM #: 17952435
This listing is for 10 mg Glass bottle

Merck - 5.08053.0001 - Mcl-1 Inhibitor II - Calbiochem

  • Item #: 17952435
  • MFR SKU: 5.08053.0001
  • Overview A cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM 142-161 for Mcl-1, but not Bcl-xL, binding (IC 50 = 310 nM vs >40 µ M; [Mcl-1] & [Bcl-xL] = 6.25 nM), displaying little inhibitory potency toward CYP450 isoforms 1A2/2D6/3A4/2C9 (IC 50 = >10 µ M). Antiproliferation potencies against 2 murine lymphoma cell lines (GI 50 = 300 nM/ MCl1-1780 & 1.1 µ M/Bcl2-1863) and 11 human cancer lines of various origins (GI 50 from 1.6 to 25 µ M) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment. Stability studies using murine and human liver microsome preparations reveal t 1/2 values of 40 min and 55 min, respectively.
  • Catalogue Number 508053
  • Brand Family Calbiochem®
  • Synonyms Myeloid Cell Leukemia-1 Inhibitor II, 7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol
  • References Richard, D.J., et al. 2013. Bioorg. Med. Chem. 21, 6642.
  • Form White powder
  • Hill Formula CHFNO
  • Chemical formula CHFNO
  • Reversible Y
  • Structure formula Image
  • Quality Level MQ100
  • Primary Target Mcl-1
  • Purity ≥ 95% by HPLC
  • Cell permeable Y
  • Ship Code Ambient Temperature Only
  • Toxicity Standard Handling
  • Storage +2° C to +8° C
  • Protect from Light Protect from light
  • Do not freeze Ok to freeze
  • Special Instructions Following reconstitution, aliquot and freeze(-20° C). Stock solutions are stable for up to 6 months at -20° C.
  • Packaged under inert gas Packaged under inert gas

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